ACTIVATION OF THE G-PROTEIN GQ 11 THROUGH TYROSINE PHOSPHORYLATION OFTHE ALPHA-SUBUNIT/

Various receptors coupled to the heterotrimeric guanine nucleotide-bin ding protein Gq/11 stimulate formation of inositol-1,4,5-trisphosphate (IP3). Activation of these receptors also induces protein tyrosine ph osphorylation. Formation of IP3 in response to stimulated receptors th at couple to Gq/11 was blocked by protein tyrosine kinase inhibitors. These inhibitors appeared to act before activation of Gq/11. Moreover, stimulation of receptors coupled to Gq/11 induced phosphorylation on a tyrosine residue (Tyr(356)) Of the G alpha(q/11) subunit, and this t yrosine phosphorylation event was essential for Gq/11 activation. Tyro sine phosphorylation of G alpha(q/11) induced changes in its interacti on with receptors. Therefore, tyrosine phosphorylation of G alpha(q/11 ) appears to regulate the activation of Gq/11 protein.